Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
1
pubmed:dateCreated
1998-6-4
pubmed:abstractText
The effects of several protease substrates or protease inhibitors on neuromuscular transmission in the isolated mouse phrenic nerve-diaphragm were studied. N-Carbobenzoxy-Gly-Gly-Arg-beta-naphthylamide (Z-GGR-N) but none of the other agents inhibited the nerve-evoked muscle contractions. By means of electrophysiological studies, Z-GGR-N was found to inhibit the amplitudes of both end-plate potentials (epps) (IC50 approximately 50 microM) and miniature end-plate potentials (mepps) but to increase the frequencies of mepps. This tripeptide could protect the nicotinic acetylcholine receptor from the irreversible inhibitory action of alpha-bungarotoxin on the mouse diaphragm. Similar to D-tubocurarine, Z-GGR-N induced tetanic fading both of nerve-evoked muscle contractions and of the amplitude of epps. Furthermore, Z-GGR-N exhibited a greater depression of the amplitudes of train-epps than those of mepps, similar to that of hexamethonium and D-tubocurarine, indicating an effect on presynaptic autoreceptors. Suramin, which could competitively reverse the inhibitory effects of non-depolarizing relaxants, acted in this study as an antagonist of all the effects of Z-GGR-N, especially those at the presynaptic site. All of these findings suggest that Z-GGR-N is a novel tripeptide possessing curare-like actions at both presynaptic and postsynaptic sites and that these actions are independent of its protease substrate property.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Feb
pubmed:issn
0014-2999
pubmed:author
pubmed:issnType
Print
pubmed:day
5
pubmed:volume
343
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
51-6
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1998
pubmed:articleTitle
Studies on curare-like action of the tripeptide carbobenzoxy-Gly-Gly-Arg-beta-naphthylamide in mouse diaphragm.
pubmed:affiliation
Institutes of Pharmacology and Toxicology, College of Medicine, National Taiwan University, Taipei.
pubmed:publicationType
Journal Article, Comparative Study, In Vitro, Research Support, Non-U.S. Gov't